SCIO-469

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 p38α MAPK 抑制剂，IC50 为 9 nM。

A potent, selective p38α MAPK inhibitor with IC50 of 9 nM; displays 10-fold selectivity for p38α over p38β, >2,000-fold selectivity over a panel of 20 other kinases, including other MAP kinases; decreases apoptosis in MDS CD34+ progenitors and leads to dose-dependant increases in erythroid and myeloid colony formation; enhances the ability of MG132 and bortezomib to induce the apoptosis of MM cells, and inhibits tumor growth in vivo.Rheumatoid Arthritis Phase 2 Discontinued.

Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.Talmapimod inhibits LPS-induced TNF-a production in human whole blood.Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.Western Blot Analysis Cell Line:MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines Concentration:100, 200 nM Incubation Time:1 hour Result:Strongly inhibits phosphorylation of p38 MAPK.

Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination. Animal Model:Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)Dosage:P.o.; twice daily orally for 14 days Administration:10, 30, 90 mg/kg Result:Dose-dependently reduced tumor growth.

Talmapimod | SCIO469 | SCIO 469

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Inflammation/Immunology

Rheumatoid Arthritis

309913-83-5

513.0035

C27H30ClFN4O3

>98% (HPLC)

10 mM in DMSO

CC1CN(C(CN1C(=O)C2=C(C=C3C(=C2)C(=CN3C)C(=O)C(=O)N(C)C)Cl)C)CC4=CC=C(C=C4)F

1H-Indole-3-acetamide, 6-chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-

(-20℃)

With Ice Pack

≥ 2 years